Avorelin (CAS No. 140703-49-7) – GnRH Agonist for Prostate Cancer Research

Description

Product Description

Avorelin (CAS No. 140703-49-7), also known as Meterelin, is a synthetic peptide agonist of gonadotropin-releasing hormone (GnRH). It is designed to mimic the activity of endogenous GnRH, providing researchers with a precise tool to study the hypothalamic-pituitary-gonadal (HPG) axis and androgen regulation. Its structure allows high receptor affinity and metabolic stability, making it suitable for both in vitro and in vivo applications.

Molecular Design and Mechanism
Avorelin has been optimized for receptor binding and reduced enzymatic degradation, resulting in an extended plasma half-life and consistent pharmacodynamics. Acting as a superagonist, Avorelin induces an initial surge of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), temporarily elevating testosterone, followed by receptor desensitization that suppresses gonadotropin release. This biphasic response is crucial for modeling androgen deprivation therapy (ADT) and endocrine feedback in preclinical studies.

Research Background
Androgen deprivation is fundamental in hormone-sensitive prostate cancer research. Avorelin allows precise modulation of LH, FSH, and testosterone levels in rodent and cell models, enabling studies on tumor growth, proliferation, apoptosis, and endocrine regulation. It is particularly valuable for examining feedback loops in the HPG axis, the effects of sustained GnRH receptor activation, and combinatorial treatment strategies.

Key Features

• High-affinity GnRH receptor agonist with enhanced metabolic stability

• Biphasic LH/FSH modulation mimicking clinical GnRH therapy

• Suitable for prostate cancer and endocrine system research

• Lyophilized peptide with high purity and batch reproducibility

• Compatible with in vitro cell assays and in vivo animal models

Research Applications

• Modeling androgen deprivation in prostate cancer studies

• Investigating hypothalamic-pituitary-gonadal axis regulation

• Evaluating hormonal feedback and downstream signaling pathways

• Studying GnRH receptor pharmacology and ligand-receptor interactions

• Preclinical testing of combinatorial therapies with ADT

• Structural and biochemical analysis of peptide-receptor interactions

• Endocrine research exploring reproductive and metabolic physiology

Advantages Over First-Generation GnRH Analogs
Compared to earlier GnRH agonists, Avorelin exhibits higher receptor selectivity, improved stability, and predictable pharmacodynamic responses. Structural optimization reduces enzymatic degradation, ensuring consistent hormone modulation. Researchers benefit from reproducible testosterone suppression and controlled LH/FSH dynamics, supporting mechanistic studies and therapeutic evaluation.

Experimental Evidence
Preclinical studies show that Avorelin:

• Induces a robust LH/FSH surge within minutes of administration

• Achieves sustained gonadotropin suppression with continuous exposure

• Reduces testosterone to castrate-equivalent levels in male rodents

• Modulates androgen-sensitive tumor growth in xenograft models

• Provides a reliable platform for combinatorial and mechanistic research

Product Specifications

Mechanism of Action

Avorelin functions through high-affinity binding to GnRH receptors on anterior pituitary gonadotrophs, triggering a controlled biphasic hormonal response:

1. Initial Activation Phase

   • Stimulates rapid secretion of LH and FSH

   • Temporarily elevates testosterone levels

   • Activates downstream androgen receptor signaling

2. Desensitization and Suppression Phase

   • Continuous receptor stimulation induces internalization and desensitization

   • Suppresses LH and FSH release, reducing testosterone production

   • Mimics clinical androgen deprivation therapy

3. Downstream Signaling Effects

   • Modulates cAMP/PKA pathways in pituitary gonadotrophs

   • Influences MAPK/ERK signaling associated with hormone production

   • Alters expression of steroidogenic enzymes in gonadal tissue

4. Research Implications

   • Enables precise control of hormonal environment in preclinical prostate cancer models

   • Supports studies of tumor regression, proliferation, and survival under androgen deprivation

   • Facilitates investigation of endocrine feedback loops and receptor pharmacodynamics

     

Side Effects

Observed effects in preclinical studies include:

• Hormonal Fluctuations: Transient testosterone surge may temporarily promote androgen-sensitive cell proliferation

• Endocrine Disruption: Prolonged administration suppresses LH/FSH, affecting reproductive hormone balance

• Injection Site Reactions: Mild erythema or inflammation in animal models

• Metabolic Effects: Altered lipid profiles and glucose metabolism reported in chronic studies

• Neurological Observations: Rare behavioral changes associated with rapid hormonal modulation

• Laboratory Safety: Handle in BSL-2 conditions; use gloves, lab coat, and eye protection; avoid inhalation or direct contact

Careful dosing, storage, and monitoring are recommended to minimize variability and adverse effects.

Disclaimer

For laboratory research use only. Not intended for human or veterinary use, diagnosis, or treatment.

Keywords

Avorelin, Meterelin, GnRH agonist, prostate cancer research, CAS 140703-49-7, androgen deprivation, pituitary-gonadal axis, endocrine research, hormone regulation peptide, preclinical tumor models

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• Temperature-controlled packaging with insurance coverage

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• Guaranteed ≥98% purity

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